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Pseudotrimezia juncifolia (Klatt) Lovo & A. Gil (Iridaceae) is a popularly known species with primarily ornamental economic interest. It has traditional uses as purgative, in conditions related to the menstrual cycle, for blood purification, as wound healing, and as anti-inflammatory. The anti-inflammatory and antinociceptive activities of the decoction from its aerial stems, corms, and stamens are described here with dereplication studies on LC-MS/MS supported by the GNPS platform, where phenolic compounds were annotated and correlated with its biological activity. The decoction was evaluated in chemical (formalin and capsaicin) and thermal (hot plate) induced nociception or carrageenan-induced inflammation in mice. Decoction (at 10, 30, or 100 mg/kg doses) significantly reduced formalin- or capsaicin-induced nociception. All doses also demonstrated an antinociceptive effect in the hot plate model increasing the time the animal spent in responding to thermal signal. Naloxone partially reversed the antinociceptive effect. An anti-inflammatory effect was observed since a reduction in cell migration, protein extravasation interleukin-1, and tumor necrosis factor production induced by carrageenan in the subcutaneous air pouch was quantified. Metabolomic analyses showed a predominance of phenolic substances, mainly flavonoids and chlorogenic acids. The literature showed that these two groups have significant anti-inflammatory and analgesic activity, and chemical data corroborate the pharmacological results observed. [ABSTRACT FROM AUTHOR]

Introduction: The chemical diversity of plants plays an essential role in the development of new drugs. However, new bioactive compound identification and isolation are challenging due to the complexity and time‐consuming nature of the traditional process. Recently, alternative strategies have become popular, such as the statistical approach to correlate compounds with biological activities, overcoming bottlenecks in bioactive natural product research. Objective: We aimed to determine bioactive compounds against resistant human melanoma cells from leaves of Aspidosperma subincanum, Copaifera langsdorffii, Coussarea hydrangeifolia, Guarea guidonea and Tapirira guianensis, using a metabolomics approach. Material and Methods: The extracts and fractions were obtained by accelerated solvent extraction (ASE) and tested against resistant melanoma cells SK‐MEL‐28 and SK‐MEL‐103. Chemical analysis was performed by high‐performance diode array detector tandem mass spectrometry (HPLC‐DAD‐MS/MS). Chemical and biological data were analysed through univariate and multivariate analysis. Results: The species present high chemical diversity, including indole alkaloids, glycosylated flavonoids, galloylquinic acid derivatives, cinnamic acid derivatives, and terpenes. The ASE fractionation separated the compounds according to the physicochemical properties; only C. langsdorffii and T. guianensis extracts were active. Both results from the chemical profile and the biological assay were treated using a metabolomics approach to identify the contribution of different classes of secondary metabolites in the viability of human melanoma cells. The analyses showed the metabolites from C. langsdorffii and T. guianensis, such as polyphenols and terpenes, were the main compounds correlated with the biological response. Conclusion: These findings afford alternative pathways that are trustworthy and less time‐consuming to identify new bioactive compounds against multidrug‐resistant human melanoma cells. We determined bioactive compounds against resistant human melanoma SK‐MEL‐28 and SK‐MEL‐103 cells from Aspidosperma subincanum, Copaifera langsdorffii, Coussarea hydrangeifolia, Guarea guidonea, and Tapirira guianensis, using ASE, HPLC‐DAD‐MS/MS, and metabolomics. The species have alkaloids, glycosylated flavonoids, galloylquinic acid derivatives, cinnamic acid derivatives, and terpenes. C. langsdorffii and T. guianensis were active; metabolomics identifies polyphenols and terpenes as the main compounds correlated with the biological response. These findings afford alternative pathways that are trustworthy and less time‐consuming to identify new bioactive compounds. [ABSTRACT FROM AUTHOR]

Essential oils, mixtures of volatile compounds, are targets of research for new antimicrobial drugs. In order to verify the potential from species of the Nectandra genus, the present study evaluated the essential oils from Nectandra amazonum , Nectandra cuspidata , Nectandra gardineri , Nectandra hihua and Nectandra megapotamica to prospect samples with high concentration of a component and its antibacterial, antibiofilm and anti- Trichomonas vaginalis activities. The essential oils from the leaves and barks were extracted by steam distillation and analyzed by gas chromatography coupled to mass spectrometry (GC–MS). The concentrations of 10 and 100 μg/mL of the essential oil were evaluated and the inhibition of bacterial growth and biofilm formation were measured, while for the evaluation of anti- T. vaginalis trophozoite viability, the concentrations from 7.8 to 1000 μg/mL were tested. Seventy-three compounds were identified from essential oils, highlighted bicyclogermacrene (up to 49.9%), elemicin (up to 42.4%), intermedeol (up to 58.2%), (E)-asarone (up to 45.9%) and (+)-α-bisabolol (up to 93.7%). The essential oil from N. megapotamica leaves presented 93.7% of (+)-α-bisabolol and demonstrated the high capacity of inhibition of the biofilm formation, in particular, against Staphylococcus aureus methicillin resistant (MRSA) and Pseudomonas aeruginosa. This sample also had significant activity against T. vaginalis (IC 50 of 98.7 μg/mL) and demonstrated cytotoxic and hemolytic effects in Vero cells and human erythrocytes. In general, the Nectandra genus revealed high chemical variability and a N. megapotamica specimen accumulated a compound on high concentration with great potential for biotechnological exploration as a new antibiofilm and anti- T. vaginalis. Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Ethnopharmacological relevance Tabebuia aurea (Silva Manso) Benth. & Hook. f. ex S. Moore is used as anti-inflammatory, analgesic and antiophidic in traditional medicine, though its pharmacological proprieties are still underexplored. In the bothropic envenoming, pain is a key symptom drove by an intense local inflammatory and neurotoxic event. The antivenom serum therapy is still the main treatment despite its poor local effects against pain and tissue injury. Furthermore, it is limited to ambulatorial niches, giving space for the search of new and more inclusive pharmacological approaches. Aim of the study evaluation of Tabebuia aurea hydroethanolic extract (HEETa) in hyperalgesia and neuronal injury induced by Bothrops mattogrossensis venom (VBm). Materials and methods Stem barks from Tabebuia aurea were extracted with ethanol and water (7:3, v/v) to yield the extract HEETa. Then, HEETa was analyzed by LC-DAD-MS and its constituents were identified. Snake venoms were extracted from adult specimens of Bothrops mattogrossensis , lyophilized and kept at −20 °C until use. Male Swiss mice, weighting 20–25 g, were used to hyperalgesia (electronic von Frey), motor impairment (Rotarod test) and tissue injury evaluation (histopatology and ATF-3 immunohistochemistry). Therefore, three experimental groups were formed: VBm (1 pg, 1 ng, 0.3 μg, 1 μg, 3 and 6 μg/paw), HEETa orally (180, 540, 720, 810 or 1080 mg/kg; 10 mL/kg, 30 min prior VBm inoculation) and VBm neutralized (VBm: HEETa, 1:100 parts, respectively). In all set of experiments a control (saline group) was used. First, we made a dose-time-response course curve of VBm's induced hyperalgesia. Next, VBm maximum hyperalgesic dose was employed to perform HEETa orally dose-time-response course curve and analyses of VBm neutralized. Paw tissues for histopathology and DRGs were collected from animals inoculated with VBm maximum dose and treated with HEETa antihyperalgesic effective dose or neutralized VBm. Paws were extract two or 72 h after VBm inoculation and DRGs, in the maximum expected time expression of ATF-3 (72 h). Results From HEETa extract, glycosylated iridoids were identified, such as catalpol, minecoside, verminoside and specioside. VBm induced a time and dose dependent hyperalgesia with its highest effect seen with 3 µg/paw, 2 h after venom inoculation. HEETa effective dose (720 mg/kg) decreased significantly VBm induced hyperalgesia (3 µg/paw) with no motor impairment and signs of acute toxicity. HEETa antihyperalgesic action starts 1.5 h after VBm inoculation and lasted up until 2 h after VBm. Hyperalgesia wasn't reduced by V Bm: HEETa neutralization. Histopathology revealed a large hemorragic field 2 h after VBm inoculation and an intense inflammatory infiltrate of polymorphonuclear cells at 72 h. Both HEETa orally and VBm: HEETa groups had a reduced inflammation at 72 h after VBm. Also, the venom significantly induced ATF-3 expression (35.37 ± 3.25%) compared with saline group (4.18 ± 0.68%) which was reduced in HEETa orally (25.87 ± 2.57%) and VBm: HEETa (19.84 ± 2.15%) groups. Conclusion HEETa reduced the hyperalgesia and neuronal injury induced by VBm. These effects could be related to iridoid glycosides detected in HEETa and their intrinsic reported mechanism. Graphical abstract fx1 [ABSTRACT FROM AUTHOR]